JP2004524323A5 - - Google Patents

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JP2004524323A5
JP2004524323A5 JP2002569189A JP2002569189A JP2004524323A5 JP 2004524323 A5 JP2004524323 A5 JP 2004524323A5 JP 2002569189 A JP2002569189 A JP 2002569189A JP 2002569189 A JP2002569189 A JP 2002569189A JP 2004524323 A5 JP2004524323 A5 JP 2004524323A5
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Prior art keywords
peptide
chelating agent
chelate conjugate
lys
gly
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Pending
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JP2002569189A
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Japanese (ja)
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JP2004524323A (en
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Priority claimed from GBGB0105224.0A external-priority patent/GB0105224D0/en
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Publication of JP2004524323A publication Critical patent/JP2004524323A/en
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Claims (11)

ＳＴレセプターに対するアフィニティをもつペプチドに四座配位キレート化剤をコンジュゲートしてなるペプチド−キレートコンジュゲートであって、該ＳＴレセプターに対するアフィニティをもつペプチドが１０〜２５残基のアミノ酸を含む、ペプチド−キレートコンジュゲート。 A peptide-chelate conjugate obtained by conjugating a tetradentate chelating agent to a peptide having affinity for ST receptor, wherein the peptide having affinity for ST receptor contains 10 to 25 amino acids Chelate conjugate. 四座配位キレート化剤が、ジアミンジオキシム、Ｎ3Ｓ配位子、Ｎ4配位子、ジアミンジフェノール及びＮ2Ｓ2配位子から選択される、請求項１記載のペプチド−キレートコンジュゲート。 Tetradentate chelating agent, a diamine dioxime, N 3 S ligands, N 4 ligands are selected from diaminediphenol and N 2 S 2 ligand of claim 1, wherein the peptide - chelate conjugates Gate. 該四座配位キレート化剤が次の式Ａのものである、請求項１又は請求項２記載のペプチド−キレートコンジュゲート。
Figure 2004524323
 式中、ＲA1−ＲA6はすべてＣＨ3であり、Ｑは−（ＣＨ2）2ＮＲ（ＣＨ2）2−であって、Ｒは、請求項１の式（Ａ）のために定義されるようなＲ基である。 The peptide-chelate conjugate according to claim 1 or 2, wherein the tetradentate chelating agent is of the following formula A.
Figure 2004524323
 Where R A1 -R A6 are all CH 3 , Q is — (CH 2 ) 2 NR (CH 2 ) 2 —, and R is defined for formula (A) of claim 1. R groups such as 該四座配位キレート化剤が次の式Ｂのものである、請求項１又は請求項２記載のペプチド−キレートコンジュゲート。
Figure 2004524323
 式中、Ｒ1及びＲ2はいずれもＨであり、Ｘはチオール保護基である。 The peptide-chelate conjugate according to claim 1 or 2, wherein the tetradentate chelating agent is of the following formula B:
Figure 2004524323
 In the formula, R 1 and R 2 are both H, and X is a thiol protecting group. 該ペプチドが配列番号１〜７から選択される、請求項１乃至請求項４のいずれか１項記載のペプチド−キレートコンジュゲート。 The peptide-chelate conjugate according to any one of claims 1 to 4, wherein the peptide is selected from SEQ ID NOs: 1-7. ペプチドと四座配位キレート化剤とのリンカー基をさらに含む、請求項１乃至請求項５のいずれか１項ペプチドーキレートコンジュゲート。 The peptide-chelate conjugate according to any one of claims 1 to 5, further comprising a linker group of a peptide and a tetradentate chelating agent. 該リンカー基が、−ポリ−Ｌｙｓ−、−ポリ−Ｇｌｕ−、−（Ｇｌｙ）2−Ｇｌｕ−（Ｌｙｓ）3−、−（Ｇｌｙ）2−Ｇｌｕ−Ｌｙｓ−Ｇｌｕ−Ｌｙｓ−、−（Ｐｈｅ）2−（ＣＨ2）5−、（Ｌｙｓ）6−Ｇｌｙ−、−（Ｇｌｙ）3−（ＤＧｌｕ）3−、及び−（Ｇｌｙ）−（アミノカプロン酸）2−から選択される、請求項６記載のペプチドコンジュゲート。 The linker group is -poly-Lys-, -poly-Glu-,-(Gly) 2 -Glu- (Lys) 3 -,-(Gly) 2 -Glu-Lys-Glu-Lys-,-(Phe) 2 - (CH 2) 5 - , (Lys) 6 -Gly -, - (Gly) 3 - (DGlu) 3 -, and - (Gly) - (aminocaproic acid) 2 - is selected from claim 6, wherein Peptide conjugates. 請求項１乃至請求項７のいずれか１項記載のペプチド−キレートコンジュゲートの四座配位キレート化剤と錯化した放射性金属を含む、金属錯体。 A metal complex comprising a radioactive metal complexed with a tetradentate chelating agent of the peptide-chelate conjugate according to any one of claims 1 to 7. 該放射性金属が99mＴｃである、請求項８記載の金属錯体。 The metal complex according to claim 8, wherein the radioactive metal is 99m Tc. ヒト投与のために好適な形態の放射性医薬組成物であって、請求項８又は請求項９記載の金属錯体を含む、組成物。 A radiopharmaceutical composition in a form suitable for human administration, comprising the metal complex of claim 8 or claim 9. 請求項１０記載の放射性医薬組成物の調製のためのキットであって、
（ｉ）請求項１乃至請求項７のいずれか１項記載のペプチド−キレートコンジュゲート、及び
（ｉｉ）還元剤
を含むキット。
A kit for the preparation of a radiopharmaceutical composition according to claim 10,
A kit comprising (i) the peptide-chelate conjugate according to any one of claims 1 to 7, and (ii) a reducing agent.
JP2002569189A 2001-03-02 2002-03-01 Tetradentate peptide-chelate conjugate for colorectal cancer diagnosis Pending JP2004524323A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0105224.0A GB0105224D0 (en) 2001-03-02 2001-03-02 Improved peptide-chelate conjugates
PCT/GB2002/000857 WO2002070018A2 (en) 2001-03-02 2002-03-01 Tetradentate peptide-chelate conjugates for colorectal cancer diagnosis

Publications (2)

Publication Number Publication Date
JP2004524323A JP2004524323A (en) 2004-08-12
JP2004524323A5 true JP2004524323A5 (en) 2005-12-22

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JP2002569189A Pending JP2004524323A (en) 2001-03-02 2002-03-01 Tetradentate peptide-chelate conjugate for colorectal cancer diagnosis

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US (1) US7608242B2 (en)
EP (1) EP1368064B1 (en)
JP (1) JP2004524323A (en)
AT (1) ATE556722T1 (en)
CA (1) CA2439579A1 (en)
ES (1) ES2385028T3 (en)
GB (1) GB0105224D0 (en)
WO (1) WO2002070018A2 (en)

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US8728478B2 (en) * 2008-09-03 2014-05-20 Board Of Trustees Of Michigan State University Immunogenic Escherichia coli heat stable enterotoxin
EP2509992B1 (en) * 2009-12-07 2015-10-14 Ironwood Pharmaceuticals, Inc. Treatments for gastrointestinal disorders
GB201016206D0 (en) * 2010-09-27 2010-11-10 Ge Healthcare Ltd Apoptosis imaging agents
GB201103696D0 (en) 2011-03-04 2011-04-20 Ge Healthcare Ltd Technetium labelled peptides
US9617305B2 (en) 2011-06-08 2017-04-11 Ironwood Pharmaceuticals, Inc. Treatments for gastrointestinal disorders
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US4545931A (en) 1983-01-03 1985-10-08 Scripps Clinic And Research Foundation Synthetic heat-stable enterotoxin polypeptide of Escherichia coli
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